Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | matrix metallopeptidase 2 (gelatinase A, 72kDa gelatinase, 72kDa type IV collagenase) | Starlite/ChEMBL | References |
Sus scrofa | ADAM17 | Starlite/ChEMBL | References |
Homo sapiens | matrix metallopeptidase 1 (interstitial collagenase) | Starlite/ChEMBL | References |
Homo sapiens | matrix metallopeptidase 9 (gelatinase B, 92kDa gelatinase, 92kDa type IV collagenase) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus multilocularis | adam 17 protease | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Schistosoma japonicum | ko:K06059 a disintegrin and metalloproteinase domain 17, putative | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus multilocularis | Blood coagulation inhibitor, Disintegrin | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Schistosoma mansoni | ADAM17 peptidase (M12 family) | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus granulosus | adam 17 protease | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus granulosus | Blood coagulation inhibitor Disintegrin | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | disintegrin and metalloproteinase | ADAM17 | 112 aa | 99 aa | 42.4 % |
Trypanosoma congolense | hypothetical protein, conserved | ADAM17 | 112 aa | 100 aa | 29.0 % |
Brugia malayi | Matrixin family protein | matrix metallopeptidase 1 (interstitial collagenase) | 403 aa | 401 aa | 27.7 % |
Plasmodium yoelii | A/G-specific adenine glycosylase, putative | ADAM17 | 112 aa | 109 aa | 24.8 % |
Echinococcus multilocularis | disintegrin and metalloproteinase | ADAM17 | 112 aa | 99 aa | 42.4 % |
Onchocerca volvulus | Putative glutaminase 3 | ADAM17 | 112 aa | 105 aa | 45.7 % |
Onchocerca volvulus | ADAM17 | 112 aa | 98 aa | 41.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | metalloprotease disintegrin 16 with thrombospondin type I motif | 0.0263 | 0.2747 | 1 |
Echinococcus multilocularis | a disintegrin and metalloproteinase with | 0.0263 | 0.2747 | 0.0466 |
Echinococcus granulosus | Blood coagulation inhibitor Disintegrin | 0.0294 | 0.3511 | 0.147 |
Echinococcus multilocularis | Blood coagulation inhibitor, Disintegrin | 0.0294 | 0.3511 | 0.147 |
Echinococcus multilocularis | adam 17 protease | 0.0557 | 1 | 1 |
Echinococcus granulosus | a disintegrin and metalloproteinase with | 0.0263 | 0.2747 | 0.0466 |
Onchocerca volvulus | Matrix metalloproteinase homolog | 0.0152 | 0 | 0.5 |
Schistosoma mansoni | ADAM17 peptidase (M12 family) | 0.0557 | 1 | 1 |
Loa Loa (eye worm) | matrixin family protein | 0.0165 | 0.0337 | 0.0961 |
Onchocerca volvulus | Matrilysin homolog | 0.0152 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0294 | 0.3511 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CL (ADMET) | = 1.5 L/hr.Kg | Clearance in Sprague-Dawley rat at 5.0 mg/kg, iv | ChEMBL. | 18242982 |
F (ADMET) | = 22 % | Oral bioavailability in Sprague-Dawley rat at 8.0 mg/kg | ChEMBL. | 18242982 |
IC50 (binding) | = 2.7 nM | Inhibition of semi purified pig TACE | ChEMBL. | 18242982 |
IC50 (binding) | = 2.7 nM | Inhibition of semi purified pig TACE | ChEMBL. | 18242982 |
IC50 (functional) | = 54 nM | Reduction of LPS-induced TNFalpha in human whole blood | ChEMBL. | 18242982 |
IC50 (functional) | = 54 nM | Reduction of LPS-induced TNFalpha in human whole blood | ChEMBL. | 18242982 |
Ki (binding) | > 2128 nM | Inhibition of MMP9 (unknown origin) | ChEMBL. | 18242982 |
Ki (binding) | > 2128 nM | Inhibition of MMP9 (unknown origin) | ChEMBL. | 18242982 |
Ki (binding) | > 3333 nM | Inhibition of MMP2 (unknown origin) | ChEMBL. | 18242982 |
Ki (binding) | > 3333 nM | Inhibition of MMP2 (unknown origin) | ChEMBL. | 18242982 |
Ki (binding) | > 4948 nM | Inhibition of MMP1 (unknown origin) | ChEMBL. | 18242982 |
Ki (binding) | > 4948 nM | Inhibition of MMP1 (unknown origin) | ChEMBL. | 18242982 |
Papp (ADMET) | = 2 10^-6 cm/s | Apparent permeability across human Caco2 cells | ChEMBL. | 18242982 |
Papp (ADMET) | = 2 10^-6 cm/s | Apparent permeability across human Caco2 cells | ChEMBL. | 18242982 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 18242982 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.